METHOD OF PRODUCING AMORPHOUS FORMS OF COMPOUNDS HAVING ANTICANCER ACTIVITY Russian patent published in 2025 - IPC C07D417/12 C07D487/04 C07D401/14 C07D213/81 C07D401/04 C07D405/04 

Abstract RU 2841137 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a process for the preparation of an amorphous form of nilotinib or nilotinib hydrochloride, comprising following steps 1) preparing a solution of the compound in dimethyl sulfoxide with concentration of 40 mg/ml; 2) while stirring in solution obtained at step 1), adding tert-butanol to concentration of up to 20 vol.%; 3) the solution obtained in step 2) is filtered through a hydrophilic filter; 4) obtained filtrate is cooled to −40 °C and lyophilized, raising temperature to 0 °C; 5) removing dimethyl sulphoxide from the dried product to a residual content of not more than 0.5%; 6) confirming the preparation of the amorphous form of nilotinib or nilotinib hydrochloride by X-ray powder diffraction.

EFFECT: obtaining an amorphous form of nilotinib or nilotinib hydrochloride with high output.

3 cl, 16 dwg, 2 tbl

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RU 2 841 137 C2

Authors

Zolotov Sergej Anatolevich

Dain Igor Aleksandrovich

Ponomarev Evgenij Sergeevich

Sazonov Georgij Konstantinovich

Zolotova Anna Sergeevna

Dates

2025-06-03Published

2023-06-21Filed